Nuciferine

SKU: orb1304271

Description

(-)-Nuciferine is a natural alkaloid isolated from Nymphaea caerulea and Nelumbo nucifera, known for its dopamine receptor antagonist activity. It is used in neuroscience research to study dopaminergic signaling and related behaviors in both in vitro and in vivo experimental models.

Research Area

Infectious Disease & Virology, Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	475-83-2
MW	295.38
Purity	99.79%
Formula	C₁₉H₂₁NO₂
SMILES	COc1cc2CCN(C)[C@@H]3Cc4ccccc4-c(c1OC)c23
Target	5-HT Receptor,Dopamine Receptor,Parasite
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.39 mM);DMSO:2.96 mg/mL (10.02 mM)

Bioactivity

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Target IC50	5-HT1A:3.2 μM (EC50)\|D5:2.6 μM (EC50)\|5-HT2C:131 nM\|5-HT2B:1 μM\|D4:2 μM (EC50)\|5-HT6:700 nM(EC50)\|D2:64 nM (EC50)\|5-HT2A:478 nM\|5-HT7:150 nM
In Vivo	In studies using rodent models to evaluate the effects of antipsychotic drugs, Nuciferine demonstrated several significant actions: it inhibited the head-twitch responses and the discriminative stimulus effects caused by a 5-HT2A agonist, effectively replaced the discriminative stimulus of clozapine, increased locomotor activity induced by amphetamine, and reduced both the locomotor activity prompted by phencyclidine (PCP) and the disruption of prepulse inhibition caused by PCP, all without causing catalepsy. When administered with cumulative doses of PCP, Nuciferine at concentrations of 1 or 3 mg/kg did not alter the PCP's effects. However, when given to animals trained to recognize clozapine, Nuciferine at a dose of 10 mg/kg induced a response comparable to clozapine (with 80.63% of the responses corresponding to the drug lever) and had an effective dose (ED50) of 5.42 mg/kg (with a 95% confidence interval between 3.09 and 9.48 mg/kg), unlike lower doses (0.1 mg/kg-3 mg/kg), which did not mimic clozapine's discriminative cue. Moreover, at 10 mg/kg, Nuciferine significantly reduced the activity rate compared to the control group treated with a vehicle, indicating a substantial therapeutic effect (p<0.001). Read more...
In Vitro	Nuciferine is a partial agonist at DD2 receptor with an activity (Emax=67% of dopamine) similar to aripiprazole (Emax=50% of dopamine). In line with its partial agonist activity, Nuciferine inhibited dopamine-induced activation of Gi with a potency similar to clozapine (Nuciferine KB=62 nM; Clozapine KB=20 nM) as determined via Schild regression analysis. The natural product Nuciferine acts as an effective inhibitor of adult worm motility. Nuciferine is effective at inhibiting both basal and 5-HT evoked motility of adult schistosomes. Nuciferine inhibits Sm.5HTRL and schistosomule with 0.24±0.04 and 0.62±0.22 μM, respectively. Read more...
Cell Research	Nuciferine is dissolved in DMSO and stored, and then diluted with appropriate medium before use. Cells are plated into 48-well plates one day before uptake is performed. Cells are washed with 0.5 mL uptake buffer (4 mM Tris, 6.25 mM HEPES, 120 mM NaCl, 5 mM KCl, 1.2 mM CaCl2, 1.2 mM MgSO4, 5.6 mM D-glucose, 1.7 mM ascorbic acid, and 1 μM pargyline, pH 7.4). Cells are incubated with 225 μL uptake buffer with or without the indicated concentration of Nuciferine for 15 minutes. After incubation, 25 μL uptake buffer containing 3H-DA and DA is added for a final concentration of 20 nM 3H-DA and 1 μM DA. Cells are incubated at 37°C for 20 minutes or for the time indicated. Nonspecific uptake is determined in the presence of 10 μM nomifensine. Uptake is terminated by aspirating uptake buffer and washing each well twice with 0.5 mL ice-cold uptake buffer. Cells are lysed in 0.1 N NaOH and transferred to vials containing 3 mL scintillation cocktail. Radioactivity is quantitated using a Beckman LS6500 counter. Data are analyzed in Graph Pad Prism 5.0. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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DopamineReceptor, Dopamine Receptor, Dopamine, D5 receptor, 5-HT7, 5HT Receptor, 5HTReceptor, 5-hydroxytryptamine Receptor, (-)-Nuciferine, 5-HT2B, 5-HT2C, 5-HT2A, 5-HT Receptor, Nuciferine, Inhibitor, inhibit, Serotonin Receptor, Sanjoinine E, VLT 049, VLT049, VLT-049

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Compound Identifiers

PubChem CID

10146 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	475-83-2
MW:	295.38
Formula:	C₁₉H₂₁NO₂

Nuciferine

Description

Research Area

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Key Properties

Bioactivity

Storage & Handling

Alternative Names

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